Antihypertensive hexa:hydro-pyrimidine thio:hydroximic acid derivs. - are 2-2-oxo or thio-4-oxo-6-carboxy hexa:hydro-1-pyrimidinyl-carbonyl-ethyl 1-thio-hydroximic acid which inhibit angiotensin I conversion

摘要

1-R5S-C(=NOH)-CHR4-CO-2-R1= -3-R3-4-oxo-5-R-6-R2OOC hexahydropyrimidine of formula (I) and their acid addn. salts, salts with bases and diastereoisomers and optically active forms are new. (R is H or opt. branched 1-6C alkyl; R1 is O or S; R2 is H or 1-6C alkyl; R3 is H or benzyloxycarbonyl; R4 is H or lower alkyl and R5 is H, lower alkyl, aryl or lower aralkyl). (I) selectively inhibit the enzyme which converts angiotensin I to the hypertensive angiotensin II and is used to treat hypertension. (I) is administered orally, parenterally, rectally, sub-liagually or by permucous route. Unit doses comprise 50-500 mg, pref. 100-250 mg, to give daily doses of about 200-800 mg. (I) may be used in association with substances having complementary, synergestic or similar activity e.g. sulphamide or thiazide diuretics, peripheral vasodilators, such as hydralazine, or a hypotensive, such as Minoxidil.